Chemical Structure : Helios degrader ALV1
CAS No.: 2438124-79-7
Catalog No.: PC-38302Not For Human Use, Lab Use Only.
Helios degrader ALV1 (ALV-03-112-01) is a small molecule degrader of the zinc-finger transcription factor Helios with IC50 of 0.55 uM in CRBN-binding TR-FRET assay, exhibits similar degradation activity towards IKZF1/2/3.
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Helios degrader ALV1 (ALV-03-112-01) is a small molecule degrader of the zinc-finger transcription factor Helios with IC50 of 0.55 uM in CRBN-binding TR-FRET assay, exhibits similar degradation activity towards IKZF1/2/3.
ALV1 recruits the E3 ubiquitin ligase substrate receptor cereblon to Helios.
ALV1 bound CRBN in vitro with greater potency than lenalidomide but less than CC-885.
ALV1 also induced CRBN-Helios dimerization in the TR-FRET assay, with greater activity than either CC-885. ALV1 degraded both Ikaros and Helios.
M.Wt | 494.932 | |
Formula | C25H23ClN4O5 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
N-(3-chloro-4-methylphenyl)-3-(3-((1-(2,6-dioxopiperidin-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl)amino)phenyl)propanamide |
1. Eric S Wang, et al. Nat Chem Biol. 2021 Jun;17(6):711-717.
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